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Page 1
A pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction.
Kaptein SJF, Goethals O, Kiemel D, Marchand A, Kesteleyn B, Bonfanti JF, Bardiot D, Stoops B, Jonckers THM, Dallmeier K, Geluykens P, Thys K, Crabbe M, Chatel-Chaix L, Münster M, Querat G, Touret F, de Lamballerie X, Raboisson P, Simmen K, Chaltin P, Bartenschlager R, Van Loock M, Neyts J. Kaptein SJF, et al. Among authors: jonckers thm. Nature. 2021 Oct;598(7881):504-509. doi: 10.1038/s41586-021-03990-6. Epub 2021 Oct 6. Nature. 2021. PMID: 34616043
Blocking NS3-NS4B interaction inhibits dengue virus in non-human primates.
Goethals O, Kaptein SJF, Kesteleyn B, Bonfanti JF, Van Wesenbeeck L, Bardiot D, Verschoor EJ, Verstrepen BE, Fagrouch Z, Putnak JR, Kiemel D, Ackaert O, Straetemans R, Lachau-Durand S, Geluykens P, Crabbe M, Thys K, Stoops B, Lenz O, Tambuyzer L, De Meyer S, Dallmeier K, McCracken MK, Gromowski GD, Rutvisuttinunt W, Jarman RG, Karasavvas N, Touret F, Querat G, de Lamballerie X, Chatel-Chaix L, Milligan GN, Beasley DWC, Bourne N, Barrett ADT, Marchand A, Jonckers THM, Raboisson P, Simmen K, Chaltin P, Bartenschlager R, Bogers WM, Neyts J, Van Loock M. Goethals O, et al. Among authors: jonckers thm. Nature. 2023 Mar;615(7953):678-686. doi: 10.1038/s41586-023-05790-6. Epub 2023 Mar 15. Nature. 2023. PMID: 36922586 Free PMC article.
Discovery of Acyl-Indole Derivatives as Pan-Serotype Dengue Virus NS4B Inhibitors.
Kesteleyn B, Bardiot D, Bonfanti JF, De Boeck B, Goethals O, Kaptein SJF, Stoops B, Coesemans E, Fortin J, Muller P, Doublet F, Carlens G, Koukni M, Smets W, Raboisson P, Chaltin P, Simmen K, Van Loock M, Neyts J, Marchand A, Jonckers THM. Kesteleyn B, et al. Among authors: jonckers thm. J Med Chem. 2023 Jul 13;66(13):8808-8821. doi: 10.1021/acs.jmedchem.3c00403. Epub 2023 Jun 30. J Med Chem. 2023. PMID: 37389813
Structural and mechanistic insights into the inhibition of respiratory syncytial virus polymerase by a non-nucleoside inhibitor.
Yu X, Abeywickrema P, Bonneux B, Behera I, Anson B, Jacoby E, Fung A, Adhikary S, Bhaumik A, Carbajo RJ, De Bruyn S, Miller R, Patrick A, Pham Q, Piassek M, Verheyen N, Shareef A, Sutto-Ortiz P, Ysebaert N, Van Vlijmen H, Jonckers THM, Herschke F, McLellan JS, Decroly E, Fearns R, Grosse S, Roymans D, Sharma S, Rigaux P, Jin Z. Yu X, et al. Among authors: jonckers thm. Commun Biol. 2023 Oct 21;6(1):1074. doi: 10.1038/s42003-023-05451-4. Commun Biol. 2023. PMID: 37865687 Free PMC article.
Molecular mechanism of respiratory syncytial virus fusion inhibitors.
Battles MB, Langedijk JP, Furmanova-Hollenstein P, Chaiwatpongsakorn S, Costello HM, Kwanten L, Vranckx L, Vink P, Jaensch S, Jonckers TH, Koul A, Arnoult E, Peeples ME, Roymans D, McLellan JS. Battles MB, et al. Among authors: jonckers th. Nat Chem Biol. 2016 Feb;12(2):87-93. doi: 10.1038/nchembio.1982. Epub 2015 Dec 7. Nat Chem Biol. 2016. PMID: 26641933 Free PMC article.
From Oxetane to Thietane: Extending the Antiviral Spectrum of 2'-Spirocyclic Uridines by Substituting Oxygen with Sulfur.
Grosse S, Tahri A, Raboisson P, Houpis Y, Stoops B, Jacoby E, Neefs JM, Van Loock M, Goethals O, Geluykens P, Bonfanti JF, Jonckers THM. Grosse S, et al. Among authors: jonckers thm. ACS Med Chem Lett. 2022 Nov 28;13(12):1879-1884. doi: 10.1021/acsmedchemlett.2c00372. eCollection 2022 Dec 8. ACS Med Chem Lett. 2022. PMID: 36518706 Free PMC article.
Discovery of JNJ-1802, a First-in-Class Pan-Serotype Dengue Virus NS4B Inhibitor.
Kesteleyn B, Bonfanti JF, Bardiot D, De Boeck B, Goethals O, Kaptein SJF, Stoops B, Coesemans E, Fortin J, Muller P, Doublet F, Carlens G, Koukni M, Smets W, Raboisson P, Chaltin P, Simmen K, Loock MV, Neyts J, Marchand A, Jonckers THM. Kesteleyn B, et al. Among authors: jonckers thm. J Med Chem. 2024 Mar 14;67(5):4063-4082. doi: 10.1021/acs.jmedchem.3c02336. Epub 2024 Feb 28. J Med Chem. 2024. PMID: 38482827
A small-molecule fusion inhibitor of influenza virus is orally active in mice.
van Dongen MJP, Kadam RU, Juraszek J, Lawson E, Brandenburg B, Schmitz F, Schepens WBG, Stoops B, van Diepen HA, Jongeneelen M, Tang C, Vermond J, van Eijgen-Obregoso Real A, Blokland S, Garg D, Yu W, Goutier W, Lanckacker E, Klap JM, Peeters DCG, Wu J, Buyck C, Jonckers THM, Roymans D, Roevens P, Vogels R, Koudstaal W, Friesen RHE, Raboisson P, Dhanak D, Goudsmit J, Wilson IA. van Dongen MJP, et al. Among authors: jonckers thm. Science. 2019 Mar 8;363(6431):eaar6221. doi: 10.1126/science.aar6221. Science. 2019. PMID: 30846569 Free PMC article.
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists.
Pieters S, McGowan D, Herschke F, Pauwels F, Stoops B, Last S, Embrechts W, Scholliers A, Mostmans W, Van Dijck K, Van Schoubroeck B, Thoné T, De Pooter D, Fanning G, Rosauro ML, Khamlichi MD, Houpis I, Arnoult E, Jonckers THM, Raboisson P. Pieters S, et al. Among authors: jonckers thm. Bioorg Med Chem Lett. 2018 Feb 15;28(4):711-719. doi: 10.1016/j.bmcl.2018.01.014. Epub 2018 Jan 16. Bioorg Med Chem Lett. 2018. PMID: 29366653
Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus.
Vendeville S, Tahri A, Hu L, Demin S, Cooymans L, Vos A, Kwanten L, Van den Berg J, Battles MB, McLellan JS, Koul A, Raboisson P, Roymans D, Jonckers THM. Vendeville S, et al. Among authors: jonckers thm. J Med Chem. 2020 Aug 13;63(15):8046-8058. doi: 10.1021/acs.jmedchem.0c00226. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32407115
29 results